Pitavastatin calcium

製品コードS1759 バッチS175903

化学情報

	Synonyms	NK-104 calcium	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₅₀H₄₆CaF₂N₂O₈
	分子量	880.98	CAS No.	147526-32-7
Solubility (25°C)*	体外	DMSO	51 mg/mL (57.89 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
in vitro	Pitavastatin significantly reduces both intracellular levels and synthesis of cholesterol esters. Pitavastatin is found to enhance LDL-receptor expression in vitro, as well as the amount of LDL binding to the LDL-receptor. Pitavastatin also exhibits more potent induction of LDL receptor mRNA expression compared with simvastatin and atorvastatin. Pitavastatin has many pleiotropic effects in vitro and in vivo, including deterring progression of atherosclerosis via inhibition of thromboxane synthesis, inhibition of migration/proliferation of vascular smooth muscle cells induced by angiotensin II, and stabilization of atherosclerotic plaque. ^[1] Pitavastatin is able to activate PPARα and induce HDL apoA-I through inducing inhibition of the Rho-signaling pathway. ^[2] Pitavastatin (1 μM) treatment for 48 h is able to enhances bone morphogenetic protein-2 BMP-2 (2.5-fold) and osteocalcin (10-fold) expression by inhibition of Rho-associated kinase in human osteoblasts^[3]. Pitavastatin inhibits growth and colony formation of liver cancer Huh-7 cells and SMMC7721 cells. It induces arrest of liver cancer cells at the G1 phase. Increased proportion of sub-G1 cells is observed after pitavastatin treatment. Pitavastatin promotes caspase-9 cleavage and caspase-3 cleavage in liver cancer cells. Pitavastatin could regulate NF-κB and anti-inflammation in hepatocellular carcinoma cells. Pitavastatin could induce autophagic cell death in glioma cells and promote sensitivity of cells to radiotherapy. It could inhibit cell proliferation and induce cell apoptosis in cholangiocarcinoma cells as well^[5].
in vivo	Pitavastatin decreases the tumor growth and improved the survival of tumor-bearing mice^[5]. Pitavastatin exerts a protective effect on dilated cardiomyopathy possibly through down-regulating the circulating and local RAS, followed by inhibition of PKCb2 phosphorylation, and consequently promoting the phosphorylation of PLB as well as the activity and the expressions of SERCA2a and RyR2, whereby heart function is preserved in the development of DCM^[6].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Huh-7 and SMMC7721
	濃度	5 μM
	反応時間	1, 2, 4, 6 days
	実験の流れ	The Huh-7 cells and SMMC7721 cells are split into 96-well dishes at 5,000 cells/well and treated with the indicated dosage of pitavastatin for 48 hours or 5 µM pitavastatin for 1, 2, 4, 6 days respectively. The cells are incubated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and formed formazan in the liver cells. Formazan is dissolved in DMSO, and the absorbance is measured at the wavelength of 570 nm. The cells treated with DMSO are used as a control group. The relative cell number of each group is calculated as pitavastatin-treated group/cell number in the DMSO-treated group.
動物実験	動物モデル	C57BL/6 mice
	投薬量	1 or 3 mg/kg/d
	投与方法	oral

参考

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カスタマーフィードバック

: Data from [Data independently produced by , , Br J Cancer, 2014, 111(8): 1562-71 ]

: Data from [Data independently produced by , , Br J Cancer, 2014, 111(8): 1562-71 ]

: Data from [Data independently produced by , , PLoS One, 2017, 12(5):e0178278]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Statin prevents cancer development in chronic inflammation by blocking interleukin 33 expression [ Nat Commun, 2024, 15(1):4099]	PubMed: 38816352
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805]	PubMed: 39581704
CRACD loss induces neuroendocrine cell plasticity of lung adenocarcinoma [ Cell Rep, 2024, 43(6):114286]	PubMed: 38796854
Gene regulatory network topology governs resistance and treatment escape in glioma stem-like cells [ Sci Adv, 2024, 10(23):eadj7706]	PubMed: 38848360
Gene regulatory network topology governs resistance and treatment escape in glioma stem-like cells [ bioRxiv, 2024, 2024.02.02.578510]	PubMed: 38370784
Cholesterol biosynthesis inhibition synergizes with AKT inhibitors in triple-negative breast cancer [ bioRxiv, 2024, 10.1101/2024.01.16.575899]	PubMed: none
Epigenetic suppression of PGC1α (PPARGC1A) causes collateral sensitivity to HMGCR-inhibitors within BRAF-treatment resistant melanomas [ Nat Commun, 2023, 14(1):3251]	PubMed: 37277330
Caffeine Supplementation and FOXM1 Inhibition Enhance the Antitumor Effect of Statins in Neuroblastoma [ Cancer Res, 2023, 83(13):2248-2261]	PubMed: 37057874
Phenotypic screening platform identifies statins as enhancers of immune cell-induced cancer cell death [ BMC Cancer, 2023, 23(1):164]	PubMed: 36803614
Phenotypic screening platform identifies statins as enhancers of immune cell-induced cancer cell death [ BMC Cancer, 2023, 23(1):164]	PubMed: 36803614

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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